Biovin P, Lecomte M C, Galand C
INSERM U.160, Hôpital Beaujon, Clichy, France.
Pathol Biol (Paris). 1988 Oct;36(8 Pt 2):1042-6.
Methylxanthines are phosphodiesterase inhibitors and are therefore capable of increasing cyclic AMP levels, thereby stimulating cyclic nucleotide-dependent protein kinases. The direct action of several xanthine derivatives on enzyme-dependent phosphorylations involving red blood cell membrane proteins was studied in vitro. Pentoxifylline and caffeine exhibited no effect on the activity of the membrane cAMP-dependent protein kinase. Conversely, methylxanthines proved capable on inhibiting cyclic nucleotide-independent protein kinases present in the membrane and cytosol. This inhibition involves competition with ATP. Comparison of the inhibitory effect of two xanthine derivatives, ie propentofylline and pentoxifylline, demonstrated significant differences. Xanthine derivatives showed no activity on red blood cell tyrosine kinase. Furthermore, three xanthines, ie caffeine, pentoxifylline and propentofylline, inhibited phosphatidylinositol kinase.
甲基黄嘌呤是磷酸二酯酶抑制剂,因此能够提高环磷酸腺苷(cAMP)水平,从而刺激环核苷酸依赖性蛋白激酶。体外研究了几种黄嘌呤衍生物对涉及红细胞膜蛋白的酶依赖性磷酸化的直接作用。己酮可可碱和咖啡因对膜cAMP依赖性蛋白激酶的活性没有影响。相反,甲基黄嘌呤被证明能够抑制存在于膜和细胞质中的非环核苷酸依赖性蛋白激酶。这种抑制涉及与三磷酸腺苷(ATP)的竞争。比较两种黄嘌呤衍生物即丙戊茶碱和己酮可可碱的抑制作用,发现存在显著差异。黄嘌呤衍生物对红细胞酪氨酸激酶没有活性。此外,三种黄嘌呤即咖啡因、己酮可可碱和丙戊茶碱抑制磷脂酰肌醇激酶。